KW-2478

KW-2478 is a novel, non-ansamycin small molecule inhibitor of heat shock protein 90 (Hsp90), designed to overcome limitations of earlier Hsp90 inhibitors such as low water solubility and toxicity[5][8]. It displays high binding affinity for Hsp90α (IC50 = 3.8 nM)[4], leading to potent antitumor activity in vitro and in vivo against various human hematological tumor cells including multiple myeloma and B-cell malignancies[1][6][8]. The mechanism involves inhibition of the Hsp90 chaperone complex, resulting in degradation of oncogenic client proteins (such as FGFR3, c-Maf, cyclin D1), suppression of transcriptional kinase Cdk9 and phosphorylated 4E-BP1 pathways—ultimately reducing tumor cell growth and survival[6]. Developed by Kyowa Hakko Kirin for hematological cancers including multiple myeloma and other B-cell malignancies, clinical development was discontinued after early-phase trials due to strategic reasons rather than safety concerns[3].

Other names

2-(2-ethyl-3,5-dihydroxy-6-(3-methoxy-4-(2-morpholinoethoxy)benzoyl)phenyl)-N,N-bis(2-methoxyethyl)acetamide819812-04-9KW-2478 free baseKW2478 free baseKW 2478 free base